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Novel D761Y and Common Secondary T790M Mutations in Epidermal Growth Factor Receptor–Mutant Lung Adenocarcinomas with Acquired Resistance to Kinase Inhibitors
TLDR
The data suggest that the type and nature of kinase inhibitor resistance mutations may be influenced by both anatomic site and mode of binding to the kinase target. Expand
ARN-509: a novel antiandrogen for prostate cancer treatment.
TLDR
ARS-509 exhibits characteristics predicting a higher therapeutic index with a greater potential to reach maximally efficacious doses in man than current AR antagonists, and offers preclinical proof of principle for ARN-509 as a promising therapeutic in bothCastration-sensitive and castration-resistant forms of prostate cancer. Expand
Dual targeting of EGFR can overcome a major drug resistance mutation in mouse models of EGFR mutant lung cancer.
TLDR
Surprisingly, it was found that only the combination of both agents together induced dramatic shrinkage of erlotinib-resistant tumors harboring the T790M mutation, because together they efficiently depleted both phosphorylated and total EGFR. Expand
Structure of Cdc42 in complex with the GTPase-binding domain of the ‘Wiskott–Aldrich syndrome’ protein
TLDR
Structural and biochemical data suggest that GBD-sequence divergence outside the CRIB motif may reflect additional regulatory interactions with functional domains that are specific to individual effectors. Expand
Loss of BAP1 function leads to EZH2-dependent transformation
TLDR
It is demonstrated that Bap1 loss in mice results in increased trimethylated histone H3 lysine 27 (H3K27me3), elevated enhancer of zeste 2 polycomb repressive complex 2 subunit (Ezh2) expression, and enhanced repression of polycomb repression complex 2 (PRC2) targets. Expand
Pharmacologic shifting of a balance between protein refolding and degradation mediated by Hsp90.
TLDR
It is found that mammalian Hsp90, in cooperation with Hsp70, p60, and other factors, mediates the ATP-dependent refolding of heat-denatured proteins, such as firefly luciferase. Expand
Chemical inhibition of N-WASP by stabilization of a native autoinhibited conformation
TLDR
The identification of wiskostatin is reported, a chemical inhibitor of the neural Wiskott-Aldrich syndrome protein (N-WASP) that interacts with a cleft in the regulatory GTPase-binding domain (GBD) of WASP in the solution structure of the complex. Expand
Sequence characteristics of functional siRNAs.
TLDR
It is shown that most functional siRNAs have characteristic sequence features and there is a 99.9% chance of designing an effective siRNA in a set of three with more than 50% knockdown efficiency in a biological readout. Expand
Inhibitors of Hedgehog Acyltransferase Block Sonic Hedgehog Signaling
TLDR
This work exploits Hedgehog acyltransferase-mediated Shh palmitoylation, a modification critical for Shh signaling, as a novel target for ShH pathway inhibition. Expand
Stressed mycobacteria use the chaperone ClpB to sequester irreversibly oxidized proteins asymmetrically within and between cells.
TLDR
A defense against stationary phase stress, oxidants, and antibiotics is revealed--the sequestration of IOPs into aggregates in association with the chaperone ClpB, followed by the asymmetric distribution of aggregates within bacteria and between their progeny. Expand
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